GW501516

GW501516 is a PPARδ receptor agonist. Endurobol was entered into clinical development as a drug candidate for metabolic diseases and cardiovascular diseases, and was abandoned in 2007 because animal testing showed that the drug caused cancer to develop rapidly in several organs.

Product information

CAS Number: 317318-70-0

Molecular Weight: 453.50

Formula: C21H18F3NO3S2

Synonym:

Endurobol

GSK-516

GW-1516

GW501516

GW-501516

GW 501516

GW1516

GW 1516

GSK 516

GSK516

Chemical Name: {4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]-2-methylphenoxy}acetic acid

Smiles: CC1=CC(=CC=C1OCC(O)=O)SCC1SC(=NC=1C)C1C=CC(=CC=1)C(F)(F)F

InChiKey: YDBLKRPLXZNVNB-UHFFFAOYSA-N

InChi: InChI=1S/C21H18F3NO3S2/c1-12-9-16(7-8-17(12)28-10-19(26)27)29-11-18-13(2)25-20(30-18)14-3-5-15(6-4-14)21(22,23)24/h3-9H,10-11H2,1-2H3,(H,26,27)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

GW501516 is shown to be the most potent and selective PPARα agonists known with an EC50 of 1.1 nM against PPARα and 1000-fold selectivity over the other human subtypes, PPARα and-γ. GW501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner.

In Vivo:

GW501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats. GW501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model. GW501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice.

References:

1. Chen W, Gao R, Xie X, Zheng Z, Li H, Li S, Dong F, Wang L. A metabolomic study of the PPARδ agonist GW501516 for enhancing running endurance in Kunming mice. Sci Rep. 2015 May 6;5:9884. doi: 10.1038/srep09884. PubMed PMID: 25943561; PubMed Central PMCID: PMC4421799.
2. Magliano DC, Penna-de-Carvalho A, Vazquez-Carrera M, Mandarim-de-Lacerda CA, Aguila MB. Short-term administration of GW501516 improves inflammatory state in white adipose tissue and liver damage in high-fructose-fed mice through modulation of the renin-angiotensin system. Endocrine. 2015 Nov;50(2):355-67. doi: 10.1007/s12020-015-0590-1. Epub 2015 Apr 9. PubMed PMID: 25854303.
3. Wang X, Sng MK, Foo S, Chong HC, Lee WL, Tang MB, Ng KW, Luo B, Choong C, Wong MT, Tong BM, Chiba S, Loo SC, Zhu P, Tan NS. Early controlled release of peroxisome proliferator-activated receptor β/δ agonist GW501516 improves diabetic wound healing through redox modulation of wound microenvironment. J Control Release. 2015 Jan 10;197:138-47. doi: 10.1016/j.jconrel.2014.11.001. Epub 2014 Nov 7. PubMed PMID: 25449811.

Products are for research use only. Not for human use.